EP3543241A4 - Preparation method for and intermediate of pyrrolo six-membered heteroaromatic ring derivative - Google Patents

Preparation method for and intermediate of pyrrolo six-membered heteroaromatic ring derivative Download PDF

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Publication number
EP3543241A4
EP3543241A4 EP17873122.0A EP17873122A EP3543241A4 EP 3543241 A4 EP3543241 A4 EP 3543241A4 EP 17873122 A EP17873122 A EP 17873122A EP 3543241 A4 EP3543241 A4 EP 3543241A4
Authority
EP
European Patent Office
Prior art keywords
pyrrolo
preparation
heteroaromatic ring
membered heteroaromatic
ring derivative
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP17873122.0A
Other languages
German (de)
French (fr)
Other versions
EP3543241B1 (en
EP3543241B8 (en
EP3543241A1 (en
Inventor
Bing Liu
Lin BIAN
Xiaohui GAO
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Jiangsu Hengrui Pharmaceutical Co Ltd
Original Assignee
Jiangsu Hengrui Medicine Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Jiangsu Hengrui Medicine Co Ltd filed Critical Jiangsu Hengrui Medicine Co Ltd
Publication of EP3543241A1 publication Critical patent/EP3543241A1/en
Publication of EP3543241A4 publication Critical patent/EP3543241A4/en
Publication of EP3543241B1 publication Critical patent/EP3543241B1/en
Application granted granted Critical
Publication of EP3543241B8 publication Critical patent/EP3543241B8/en
Active legal-status Critical Current
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Rheumatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
EP17873122.0A 2016-11-23 2017-11-22 Preparation method for and intermediate of pyrrolo six-membered heteroaromatic ring derivative Active EP3543241B8 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201611035019 2016-11-23
PCT/CN2017/112237 WO2018095320A1 (en) 2016-11-23 2017-11-22 Preparation method for and intermediate of pyrrolo six-membered heteroaromatic ring derivative

Publications (4)

Publication Number Publication Date
EP3543241A1 EP3543241A1 (en) 2019-09-25
EP3543241A4 true EP3543241A4 (en) 2020-06-10
EP3543241B1 EP3543241B1 (en) 2022-09-07
EP3543241B8 EP3543241B8 (en) 2022-10-12

Family

ID=62195415

Family Applications (1)

Application Number Title Priority Date Filing Date
EP17873122.0A Active EP3543241B8 (en) 2016-11-23 2017-11-22 Preparation method for and intermediate of pyrrolo six-membered heteroaromatic ring derivative

Country Status (11)

Country Link
US (2) US10851100B2 (en)
EP (1) EP3543241B8 (en)
JP (1) JP6937828B2 (en)
KR (1) KR20190084299A (en)
CN (1) CN108884100B (en)
AU (1) AU2017366400B2 (en)
BR (1) BR112019008812A2 (en)
CA (1) CA3040981A1 (en)
MX (1) MX2019005319A (en)
TW (1) TWI771342B (en)
WO (1) WO2018095320A1 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111205290B (en) * 2018-11-22 2021-10-08 江苏恒瑞医药股份有限公司 Crystal form of JAK kinase inhibitor and preparation method thereof
CN113698404B (en) * 2020-05-21 2023-06-16 江苏恒瑞医药股份有限公司 Hexahydrocyclopenta [ c ] pyrrole-2 (1H) -formamide compound with low solvent residue and preparation method thereof
CN114591321A (en) * 2020-12-04 2022-06-07 广州费米子科技有限责任公司 Aza-and-cyclic compounds, method for the production thereof and use thereof
CN112679411B (en) * 2020-12-31 2022-04-01 上海再启生物技术有限公司 Preparation method of chiral 5- (methylamino) hexahydrocyclopenta [ c ] pyrrole-2 (1H) -Boc methanesulfonate
TW202320788A (en) * 2021-08-12 2023-06-01 大陸商江蘇恒瑞醫藥股份有限公司 Pyrrole six-membered heteroaromatics for the treatment or prevention of anti-host disease

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012058645A1 (en) * 2010-10-29 2012-05-03 Biogen Idec Ma Inc. Heterocyclic tyrosine kinase inhibitors
EP2796460A1 (en) * 2011-12-21 2014-10-29 Jiangsu Hengrui Medicine Co. Ltd. Pyrrole six-membered heteroaryl ring derivative, preparation method therefor, and medicinal uses thereof
WO2015083028A1 (en) * 2013-12-05 2015-06-11 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
EP3006445A1 (en) * 2013-06-07 2016-04-13 Jiangsu Hengrui Medicine Co. Ltd. Bisulfate of janus kinase (jak) inhibitor and preparation method therefor
WO2016116025A1 (en) * 2015-01-20 2016-07-28 南京明德新药研发股份有限公司 Jak inhibitor

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA006227B1 (en) 1999-12-10 2005-10-27 Пфайзер Продактс Инк. PIRROLO(2,3-d)PYRIMIDINE COMPOUNDS
CA2412560C (en) * 2000-06-26 2008-12-30 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine compounds as immunosuppressive agents
CN101230058A (en) 2007-01-23 2008-07-30 上海恒瑞医药有限公司 Bicycle aza alkyl derivative, preparation method and use in medicine thereof
JP2011500806A (en) 2007-10-25 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション Therapeutic compounds
TWI466885B (en) * 2009-07-31 2015-01-01 Japan Tobacco Inc Nitrogen-containing spiro cyclic compounds and pharmaceutical use thereof
WO2016024185A1 (en) * 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012058645A1 (en) * 2010-10-29 2012-05-03 Biogen Idec Ma Inc. Heterocyclic tyrosine kinase inhibitors
EP2796460A1 (en) * 2011-12-21 2014-10-29 Jiangsu Hengrui Medicine Co. Ltd. Pyrrole six-membered heteroaryl ring derivative, preparation method therefor, and medicinal uses thereof
EP3006445A1 (en) * 2013-06-07 2016-04-13 Jiangsu Hengrui Medicine Co. Ltd. Bisulfate of janus kinase (jak) inhibitor and preparation method therefor
WO2015083028A1 (en) * 2013-12-05 2015-06-11 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
WO2016116025A1 (en) * 2015-01-20 2016-07-28 南京明德新药研发股份有限公司 Jak inhibitor

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO2018095320A1 *

Also Published As

Publication number Publication date
JP6937828B2 (en) 2021-09-22
JP2019535717A (en) 2019-12-12
US20190308972A1 (en) 2019-10-10
CA3040981A1 (en) 2018-05-31
EP3543241B1 (en) 2022-09-07
KR20190084299A (en) 2019-07-16
US10851100B2 (en) 2020-12-01
MX2019005319A (en) 2019-06-20
EP3543241B8 (en) 2022-10-12
EP3543241A1 (en) 2019-09-25
TW201837039A (en) 2018-10-16
CN108884100B (en) 2021-04-06
US20210024521A1 (en) 2021-01-28
BR112019008812A2 (en) 2019-07-16
AU2017366400A1 (en) 2019-05-23
CN108884100A (en) 2018-11-23
TWI771342B (en) 2022-07-21
WO2018095320A1 (en) 2018-05-31
AU2017366400B2 (en) 2021-08-26

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